Privileged structure-based ligands for melanocortin receptors-tetrahydroquinolines, indoles, and aminotetralines |
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| Authors: | Fisher Matthew J Backer Ryan T Husain Saba Hsiung Hansen M Mullaney Jeffrey T O'Brian Thomas P Ornstein Paul L Rothhaar Roger R Zgombick John M Briner Karin |
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| Institution: | Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46258, USA. fisher_matthew_j@lilly.com |
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| Abstract: | Substitution of the aryl sulfonamide moiety contained in MC4 agonist 1 with bicyclic heterocycles and aminotetralines produced compounds with MC4 activity. The heterocycles represent alternative privileged structures to that contained in 1. Compounds in which the polar group of the privileged structure was displayed in an endocyclic fashion were not as active as the parent agonist 1, while those with an exocyclic polar group afforded activity competitive with 1. |
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